Dual degradation mechanism of GPX4 degrader in induction of ferroptosis exerting anti-resistant tumor effect

C Wang, C Zheng, H Wang, S Shui, H Jin, G Liu… - European Journal of …, 2023 - Elsevier
induce ferroptosis of HT1080 cells via GPX4 inhibition and degradation. In summary, our
data revealed that the GPX4 degrader 8e … GPX4 inhibitor RSL3. Thus, an efficient strategy to …

A potent GPX4 degrader to induce ferroptosis in HT1080 cells

H Song, J Liang, Y Guo, Y Liu, K Sa, G Yan… - European Journal of …, 2024 - Elsevier
… Unlike the previously reported GPX4 degrading agents, this study reported the potent
GPX4 PROTACs based on cIAP-E3 ligase for the first time. We found that when the linker was …

Intracellular delivery of glutathione peroxidase degrader induces ferroptosis in vivo

T Luo, Q Zheng, L Shao, T Ma, L Mao… - Angewandte …, 2022 - Wiley Online Library
… peroxidase 4 (GPX4) and induces cancer cell ferroptosis. We … GPX4 degrader, dGPX4,
can deplete tumor cell GPX4 via … of ferroptosis induction efficiency compared to that of GPX4

Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells

H Wang, C Wang, B Li, C Zheng, G Liu, Z Liu… - European Journal of …, 2023 - Elsevier
… In summary, a potent and safe compound DC-2 has been found to induce GPX4 degradation
and subsequent ferroptosis. This study may have an important implication for the design of …

ZX703: a small-molecule degrader of GPX4 inducing ferroptosis in human cancer cells

M Hu, X Li, L Wang, Y Zhang, Y Sun… - ACS Medicinal …, 2024 - ACS Publications
… , we investigated the kinetics of GPX4 degradation induced by 5i in … GPX4 was degraded
after 6 h treatment with 5i. Remarkably, over 80% of the GPX4 protein was effectively degraded

PDTAC: targeted photodegradation of GPX4 triggers ferroptosis and potent antitumor immunity

S Liu, X Zhao, S Shui, B Wang, Y Cui… - Journal of Medicinal …, 2022 - ACS Publications
… (26) Here, we designed two PDTACs by conjugating VPF with GPX4-targeting … nor degrading
activity. These PDTACs can selectively degrade GPX4 and dominantly induce ferroptotic

SMG9 drives ferroptosis by directly inhibiting GPX4 degradation

L Han, L Bai, X Fang, J Liu, R Kang, D Zhou… - Biochemical and …, 2021 - Elsevier
… For example, the activation of NMD provides protection against apoptosis induced by
chemotherapeutic drugs by degrading the mRNA of pro-apoptotic genes (eg, growth arrest-specific …

[HTML][HTML] Acid sphingomyelinase-dependent autophagic degradation of GPX4 is critical for the execution of ferroptosis

F Thayyullathil, AR Cheratta, A Alakkal… - Cell death & …, 2021 - nature.com
… role in ferroptosis inducers (FINs)-induced glutathione peroxidase 4 (GPX4) degradation and
ferroptosis … Era-induced features of autophagy, GPX4 degradation, LPO, and subsequent …

[HTML][HTML] Identification of a small molecule as inducer of ferroptosis and apoptosis through ubiquitination of GPX4 in triple negative breast cancer cells

Y Ding, X Chen, C Liu, W Ge, Q Wang, X Hao… - Journal of hematology & …, 2021 - Springer
… of inducing ferroptosis through ubiquitination of GPX4. Moreover, the mechanism of GPX4
… inactivation and iron oxidation [37] and FIN56 induced ferroptosis by degrading GPX4 with …

Targeting GPX4 in human cancer: Implications of ferroptosis induction for tackling cancer resilience

J Lee, JL Roh - Cancer Letters, 2023 - Elsevier
GPX4 inhibition and ferroptosis induction [18]. Several reviews have summarized GPX4
regulation and ferroptosis induction … was discovered as a highly efficacious GPX4 degrader, 2–3 …